Abstract: OBJECTIVE To study the pharmacokinetic behavior of NFX-SBE-β-CD complex in rats. METHODS NFX and its SBE-β-CD complex were administered orally to two groups of rats, respectively. The plasma NFX concentrations at different time following administration were determined by HPLC to estimate the main pharmacokinetic parameters. RESULTS The Cmax values for NFX and its SBE-β-CD complex were (3.57±2.46)μg·mL^-1 and (6.92±4.03)μg·mL^-1, AUC0-∞ were (9.94±5.72)μg·h·mL^-1 and (14.63±5.39)μg·h·mL^-1, respectively. The C_max and AUC_0-∞ values for the complex were significantly greater than those of NFX(P<0.05). The relative bioavailability of the NFX complex was 147.2%. CONCLUSION The absorption rate, especially the plasma drug peak concentration and bioavailability of the drug in rats were significantly increased by the complex formation of NFX with SBE-β-CD.